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Hit to lead optimization of pyrazolo[1,5-a]pyrimidines as B-Raf kinase inhibitors. 2009
Ariamala Gopalsamy, and
Greg Ciszewski, and
Mengxiao Shi, and
Dan Berger, and
Yongbo Hu, and
Frederick Lee, and
Larry Feldberg, and
Eileen Frommer, and
Steven Kim, and
Karen Collins, and
Donald Wojciechowicz, and
Robert Mallon
Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. gopalsa@wyeth.com
Our continued effort towards optimization of the pyrazolo[1,5-a]pyrimidine scaffold as B-Raf kinase inhibitors is described. Structure guided design was utilized to introduce kinase hinge region interacting groups in the 2-position of the scaffold. This strategy led to the identification of lead compound 9 with enhanced enzyme and cellular potency, while maintaining good selectivity over a number of kinases.
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Robert Mallon
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